Negative health and disease states are associated with vitamin deficiency. Optimal vitamin concentrations are required by the body to properly eliminate toxins from the body, promote the proper functioning of the digestive and cardiovascular systems, and provide a feeling of wellness. In addition to formal deficiency, an over consumption of one vitamin can produce an out of balance condition creating a deficiency in another vitamin, even if that vitamin is not formally low. Enhanced concentrations of some vitamins are also known to reduce or eliminate the symptoms of some chronic conditions.
Vitamin A is oil-soluble and plays a vital role in bone growth, reproduction, and immune system health. It also helps the skin and mucous membranes repel bacteria and viruses more effectively. Vitamin A is essential to healthy vision, and may slow declining retinal function in people with retinitis pigmentosa.
The B complex vitamins are water-soluble and include Vitamins B1-B3, B5-B7, B9, and B12. The B complex vitamins assist in converting food into energy and in repairing and maintaining tissues and cellular structures.
Vitamin D3 is oil-soluble and assists the body in absorbing calcium and phosphorous and helps to prevent bone disorders. The body makes Vitamin D when exposed to sunlight.
Vitamin C (ascorbic acid) is water-soluble and serves as an antioxidant that deactivates free radicals, and thus assists in repairing and building tissues. When taken orally in larger doses, including the upper limit of 2,000 mg per day, Vitamin C can result in acid reflux.
Vitamin E is oil-soluble includes the tocotrienols (alpha, beta, gamma, and delta isomers) and the tocopherols (alpha, beta, gamma, and delta isomers), which are all oil-soluble. All tocotrienol and tocopherol isomers (thus, all forms of Vitamin E) have some antioxidant activity due to an ability to donate a hydrogen atom (a proton plus electron) to an oxygen radical—thus deactivating the radical by forming an —OH (alcohol) group. The critical chemical structural difference between the tocotrienol and tocopherol forms of Vitamin E is that the tocopherols have saturated side chains, while the tocotrienols have unsaturated isoprenoid side chains with three double bonds. The different tocotrienol isomers demonstrate different bioavailability and efficacy depending on the type of antioxidant performance being measured. Conventionally, alpha-tocopherol has been the preferred form of “Vitamin E”, as this oil-soluble tocopherol isomer is credited with having the highest antioxidant biological activity and is preferentially absorbed and accumulated in humans when orally consumed.
Vitamins K1 and K2 are oil-soluble and are essential for helping the body respond to injuries. K1 and K2 are active in regulating blood clotting and assisting in the transport of calcium throughout the body.
The carotenoids lutein, zeaxanthin, lycopene, and beta carotene are oil-soluble and are believed to provide antioxidant properties, possibly in part by activating Nrf2, a cellular regulator of antioxidant production.
Milk thistle is presently believed to function as an antioxidant and an anti-inflammatory. Milk thistle is also reported to increase toxin excretion from the liver.
Vitamins are conventionally introduced to the bloodstream in multiple ways. Vitamins taken orally are adsorbed at different rates due to different factors. For example, on average about 10% to 20% of a solid vitamin tablet taken orally is adsorbed. This can be increased to about 30% with an orally taken gel capsule and to about 50% with a conventional intra-oral (sublingual). Injections provide from approximately 90% to 100% adsorption, but are not commonly used for vitamins unless a deficiency has caused acute illness.
While injections provide immediate and nearly total adsorption into the bloodstream, unless the injection is continued for an extended period, thus becoming an infusion, the timeframe in which the vitamins are available to the living cells may be limited. If the living cells can only adsorb a relatively low amount of the vitamin per unit time, the high, but time limited vitamin concentration in the blood may not translate into the desired cellular concentration of the vitamin.
The health benefits of supplying larger doses of vitamins and minerals to the bloodstream than available through conventional oral formulations have been recognized for over 30 years. The most documented history likely surrounds the “Myers cocktail”, which has been developed and used since at least the 1960's. The cocktail was successfully used to treat and control chronic problems including fatigue, depression, chest pain, and heart palpitations. More recent formulations of the cocktail have been used to successfully treat asthma, acute migraines, chronic fatigue syndrome, fibromyalgia, acute muscle spasm, upper respiratory tract infections, chronic sinusitis, and seasonal allergies. The Myers cocktail generally includes magnesium chloride, calcium gluconate, calcium pantothenate, Vitamin C, and some B vitamins.
Intravenous (IV) administration of the Myers cocktail achieves blood serum vitamin concentrations not possible with conventional oral administration. For example, with Vitamin C a blood concentration limitation exists irrespective of the oral dose. As the oral dose of Vitamin C is increased, the blood serum concentration of Vitamin C approaches an upper limit due to gastrointestinal saturation and a marked increase in urinary excretion. For example, when daily Vitamin C intake was increased from 200 mg/day to 2,500 mg/day, the plasma concentration only increased by 25%, from 1.2 mg/dL to 1.5 mg/dL. The highest blood serum Vitamin C level observed after oral administration of pharmacological doses was 9.3 mg/dL. In contrast, IV administration of 50 g/day of Vitamin C provided a mean peak plasma level of 80 mg/dL. Similarly, conventional oral administration of magnesium results in little or no change in blood serum magnesium concentration, while IV administration can double or triple the serum levels for short periods of time.
The concentration of nutrients available to the cells, thus blood serum levels, significantly affect the effect of the nutrients on the cells. For example, the antiviral effect of Vitamin C has been demonstrated at a concentration of 10-15 mg/dL in blood serum, a concentration that is not achievable through conventional oral administration. Thus, the IV administration of nutrients, through the production of a marked, though short-lived, increase in blood serum concentration, is believed to provide a window of opportunity for ailing cells to take up needed nutrients. It has been demonstrated that patients who receive a series of IV injections become progressively healthier, and after becoming healthier, the interval between injections can be increased until they are no longer needed.
FIG. 1A and FIG. 1B represent a liposome 100 having a double wall (bilayer) of phospholipids formed from a hydrophilic exterior wall 120 and a hydrophilic interior wall 125. The interior of the double wall 110 is hydrophobic. The hydrophilic interior wall 125 forms a capsule interior 130, to form what may be referred to as a “water-core” liposome. Liposomes may be thought of as small, fluid-filled capsules where the wall of the capsule is formed from two layers of a phospholipid. As phospholipids make up the outer membranes of living cells, the liposome 100 can be thought of as having an outer, permeable membrane wall like a cell, but without a nucleus or the other components of a living cell within the capsule interior 130. The outer and inner walls 120, 125 of the represented liposome 100 are water-soluble, while the interior of the wall 125 is fat-soluble. A common phospholipid used to form liposomes is phosphatidylcholine (PC), a material found in lecithin.
When introduced to the body, liposomes are known to deliver their internal contents to living cells through one of four methods: adsorption, endocytosis, lipid exchange, and fusion. In adsorption, the outer wall of the liposome sticks to the living cell and releases its contents through the outer wall of the living cell into the living cell. In endocytosis, the living cell consumes the liposome, thus bringing the entire liposome into the cell. The cell then dissolves the outer wall of the liposome and releases the liposome contents into the interior of the living cell. In lipid exchange, the liposome opens in close proximity to the living cell and the living cell takes in the localized high concentration of liposome interior. In fusion, the outer wall of the liposome becomes part of the outer wall of the living cell, thus carrying the contents of the liposome into the enlarged living cell. These pathways allow for a potential 100% transfer of the interior contents of the liposome to the interior of the living cell, if the liposome can be brought into close proximity to the cell and is properly constructed to interact with the target cell.
FIG. 2 represents a flattened side view of the double wall (bilayer) of phospholipids that forms the liposome. The phospholipids have polar, hydrophilic “heads” and less polar, relatively hydrophobic “tails”. In this representation, the heads form the top and bottom of the bilayer, with the tails forming the interior middle. Oil-soluble compounds can reside between the top and bottom layers within the interior area occupied by the tails.
FIG. 3 represents a micelle 300 having a single wall of phospholipids (monolayer) forming a hydrophilic exterior 320 and a hydrophobic interior 310 lacking the hydrophilic capsule interior of a liposome. Thus, in relation to a liposome, a micelle lacks a bilayer and does not provide the capsule interior that can contain a water-soluble, hydrophilic core composition. The micelle 300 may be thought of as the outer wall of a liposome without the inner wall providing for a capsule interior. Polyethylene glycol modified vitamin E, such as tocopheryl polyethylene glycol succinate 1000 (TPGS), may be used to form micelles in water as the TPGS has a water-soluble head and an oil-soluble tail.
FIG. 4 represents a monolayer surfactant where the oil component is associated with the hydrophobic tails of a surfactant. In this representation, the surfactant has formed a circular shape, thus encircling the oil component and approximating a relatively large, expanded micelle, but that is not required for the oil component to associate with the hydrophobic tails.
The present invention avoids or ameliorates at least some of the disadvantages of conventional oral and intravenous delivery systems for nutrient supplementation of a living organism.